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Vitamin E succinate polyethylene glycol nano-micelle as well as preparation method and application thereof

A technology of polyethylene glycol and succinate, applied in nanotechnology, nanotechnology, nanomedicine, etc., can solve the problems of preparing micelles without TPGS, and achieve the effect of good stability

Pending Publication Date: 2020-12-01
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In the prior art, most of the TPGS is chemically bonded with other substances to form micelles, and there is no report of preparing micelles from TPGS itself

Method used

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  • Vitamin E succinate polyethylene glycol nano-micelle as well as preparation method and application thereof
  • Vitamin E succinate polyethylene glycol nano-micelle as well as preparation method and application thereof
  • Vitamin E succinate polyethylene glycol nano-micelle as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Weigh 5 mg of TPGS with a polyethylene glycol molecular weight of 1000 Da, put it in a beaker and dissolve it with 200 μL of methanol to obtain solution B; then add the obtained solution B dropwise to deionized water under stirring conditions, and stir in a fume hood for 12 hours. The organic solvent and impurities were removed by dialysis to obtain a solution C; finally, the obtained solution C was filtered through a 0.22 μm microporous membrane to obtain a TPGS nanomicelle solution.

Embodiment 2

[0053] Weigh 5 mg of TPGS with a polyethylene glycol molecular weight of 1000 Da, put it in a beaker and dissolve it with 200 μL ethanol to obtain solution B; then add the obtained solution B dropwise to deionized water under stirring conditions, and stir in a fume hood for 12 hours. The organic solvent and impurities were removed by dialysis to obtain a solution C; finally, the obtained solution C was filtered through a 0.22 μm microporous membrane to obtain a TPGS nanomicelle solution.

Embodiment 3

[0055] Weigh 5 mg of TPGS with a polyethylene glycol molecular weight of 2000 Da, put it in a beaker and dissolve it with 200 μL tetrahydrofuran to obtain solution B; then add the obtained solution B dropwise to deionized water under stirring conditions, and stir in a fume hood for 12 hours. The organic solvent and impurities were removed by dialysis to obtain a solution C; finally, the obtained solution C was filtered through a 0.22 μm microporous membrane to obtain a TPGS nanomicelle solution.

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Abstract

The invention discloses a vitamin E succinate polyethylene glycol nano-micelle as well as a preparation method and application thereof. According to the invention, vitamin E succinate polyethylene glycol (TPGS) is prepared into the nano-micelle with an extremely simple process by combining a thin film hydration method and a self-assembly technology, the particle size of the TPGS nano-micelle is about 100 nm, and the TPGS nano-micelle has a strong killing effect on human cervical cancer cells and has small toxic and side effects on normal cells. The in-vivo circulation time can be prolonged through intravenous injection, and the nano-micelle has an obvious tumor inhibition effect on cervical cancer model mice.

Description

technical field [0001] The invention belongs to the field of nano drug preparations, in particular to a nano drug preparation of vitamin E succinate polyethylene glycol. Background technique [0002] Amphiphilic polymers containing hydrophobic blocks and hydrophilic blocks can self-assemble into micelles under certain conditions, and have good in vivo and in vitro stability and biocompatibility, so they have long been used as a variety of poorly soluble drugs Carriers or prodrugs. Among them, vitamin E succinate polyethylene glycol (D-α-tocopherol polyethylene glycolsuccinate, abbreviated as TPGS, CAS#: 9002-96-4, molecular formula (C 2 h 4 O)nC 33 h 54 o 5 ) is formed by the esterification of natural vitamin E succinate (VES) and polyethylene glycol (PEG). The relative molecular mass of TPGS is about 1513, the hydrophilic-lipophilic equilibrium HLB value is about 13-17, and the critical micelle concentration is about 0.02% (w / w). The acute oral median lethal dose (LD...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/22A61K31/355A61P35/00B82Y5/00
CPCA61K9/1075A61K31/355A61K47/22A61P35/00B82Y5/00
Inventor 侯振清姜贝莉范仲雄侯鲁
Owner XIAMEN UNIV